GPR35 Agonist

Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.

CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a K_i of 12.8 nM.

Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC₅₀ of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties.

Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

Kynurenic acid-d₅ is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.

Pamoic acid disodium is a potent GPR35 agonist with an EC₅₀ value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC₅₀ values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.

GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC₅₀s of 26 and 3.2 nM in the β-arrestin and Ca²⁺ release assay, respectively.

Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide.

GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC₅₀ of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4.

Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase with an IC₅₀ value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC₅₀ of 5.3 µM.